[Blockade of HERG K+ channels expressed in Xenopus oocytes by antipsychotic agents].

Author: DegtiarV Ie, Naid'onovV G, OsypenkoV M, ShubaIa M

Paper Details 
Original Abstract of the Article :
We have investigated the effects of neuroleptic agents, haloperidol, pimozide and fluspirilen, that are used in clinics to treat psychiatric disorders, but reportedly have proarrhythmic side effects, on HERG-encoded K+ channels responsible for the rapid component of cardiac delayed rectifier K+ curr...See full text at original site
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引用元:
https://pubmed.ncbi.nlm.nih.gov/11296551

データ提供:米国国立医学図書館(NLM)

The Impact of Antipsychotic Agents on Cardiac Function

In the realm of [cardiology], it's crucial to understand the delicate interplay between medications and the heart's electrical rhythm. This study delves into the effects of antipsychotic agents, specifically haloperidol, pimozide, and fluspirilen, on HERG-encoded K+ channels, which play a pivotal role in the heart's repolarization process. Think of these channels as the gatekeepers of the heart's electrical signals, ensuring a smooth and rhythmic beat. Like a camel navigating a desert, these channels must function flawlessly for the heart to operate efficiently.

Unveiling the Hidden Side Effects of Antipsychotics

The researchers employed [electrophysiology] techniques using Xenopus oocytes to investigate how these antipsychotic agents interacted with the HERG channels. They discovered that these agents blocked the channels in a voltage-dependent manner, meaning their effectiveness increased with depolarization. It's like a camel encountering a sandstorm—the stronger the wind, the more difficult it becomes to navigate. The IC50 values, which represent the concentration needed to block half of the channels, were determined for each agent. This data reveals that haloperidol was the most potent blocker, followed by pimozide and fluspirilen.

The Implications for Cardiac Safety

The study found that these antipsychotics didn't affect the HERG channels' activation or inactivation properties, meaning they didn't change the channels' natural opening and closing behaviors. However, the blockade of HERG channels can lead to a slower repolarization phase of the cardiac action potential, causing a prolonged QT interval on an electrocardiogram (ECG). Think of the ECG as a map of the heart's electrical activity. A prolonged QT interval is like a detour on the heart's electrical highway, increasing the risk of irregular heart rhythms. This study provides a valuable insight into the potential proarrhythmic actions of antipsychotic agents and highlights the need for careful monitoring of patients receiving these medications.

Dr. Camel's Conclusion

This research illuminates the potential consequences of antipsychotic use on the heart's rhythm, emphasizing the need for vigilance in managing patients. It's like a camel navigating a desert, being mindful of the obstacles that might appear. Understanding these risks allows us to better predict and manage potential cardiac issues in individuals taking these medications.
Date :
  1. Date Completed 2002-06-18
  2. Date Revised 2014-11-20
Further Info :

Pubmed ID

11296551

DOI: Digital Object Identifier

11296551

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PICO Info
in preparation
Languages

Ukrainian

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